- Imidazole carbene ligand with amide remote basic functional group as well as synthesis method and application thereof
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The invention discloses an imidazole carbene ligand with an alkaline remote functional group, which is a compound shown as a formula (1). The ligand and gold can form a stable metal complex used for catalyzing cyclization reactions, rearrangement reactions, nucleophilic addition reactions and the like. The invention provides a synthetic route of the novel imidazole carbene ligand and a metal complex thereof, achieving simple and efficient alkyne nucleophilic addition. The NHC-Au catalyst is provided with a Lewis acid activation center taking gold as a center and an alkali activation center taking a basic group as a center, and a hindered Lewis acid-base pair can be formed by utilizing a unique linear structure of a monovalent gold complex (ligand-gold-substrate), so that beneficial interaction between the basic functional group and a nucleophilic reagent or substrate is realized, and dual synergistic activation effects of a catalytic system on a reaction transition state are achieved.
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Paragraph 0041; 0049-0052
(2019/12/02)
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- Pyrido[1,2-a][1,2,4]triazole carbene ligand as well as synthesis method and application thereof
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The invention provides a pyrido[1,2-a][1,2,4]triazole carbene ligand as well as a synthesis method and application thereof. A pyrido[1,2-a][1,2,4]triazole carbene-gold complex formed from the pyrido[1,2-a] [1,2,4]triazole carbene ligand shown as a formula V and gold can be applied to alkyne catalytic addition reaction, has Lewis acid/alkali double activation centers, and can depend on the 'synergistic activation effect' of the double activation centers, so that the catalytic effect which cannot be achieved or cannot be achieved by a conventional ligand is achieved, and the addition reaction ofa nucleophilic reagent to multiple bonds can be greatly accelerated.
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Paragraph 0037; 0045-0048
(2019/12/02)
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- Amide Effects in C?H Activation: Noncovalent Interactions with L-Shaped Ligand for meta Borylation of Aromatic Amides
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A new concept for the meta-selective borylation of aromatic amides is described. It has been demonstrated that while esters gave para borylations, amides lead to meta borylations. For achieving high meta selectivity, an L-shaped bifunctional ligand has been employed and engages in an O???K noncovalent interaction with the oxygen atom of the moderately distorted amide carbonyl group. This interaction provides exceptional control for meta C?H activation/borylation.
- Bisht, Ranjana,Hoque, Md Emdadul,Chattopadhyay, Buddhadeb
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supporting information
p. 15762 - 15766
(2018/11/10)
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- Identification of new γ-hydroxybutenolides that preferentially inhibit the activity of mPGES-1
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Microsomal prostaglandin E2 synthase-1 (mPGES-1) has been recognized as novel, promising drug target for anti-inflammatory and anticancer drugs. mPGES-1 catalyzes the synthesis of the inducible prostaglandin E 2 in response to pro-inflammatory stimuli, rendering this enzyme extremely interesting in drug discovery process owing to the drastic reduction of the severe side effects typical for traditional non-steroidal anti-inflammatory drugs. In the course of our investigations focused on this topic, we identified two interesting molecules bearing the γ- hydroxybutenolide scaffold which potently inhibit the activity of mPGES-1. Notably, the lead compound 2c that inhibited mPGES-1 with IC50 = 0.9 μM, did not affect other related enzymes within the arachidonic acid cascade.
- De Simone, Rosa,Bruno, Ines,Riccio, Raffaele,Stadler, Katharina,Bauer, Julia,Schaible, Anja M.,Laufer, Stefan,Werz, Oliver
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p. 5012 - 5016
(2012/09/22)
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